Compound with anti-tumor activity, preparation method therefor, and use thereof

Abstract

The present invention relates to a compound of chemical formula (I), and further relates to a preparation method therefor and use thereof. Pharmacological experiment results show that the compound of the present invention has excellent anti-tumor activity, good stability, low toxicity, and broad-spectrum efficacy, and can be used as an anti-tumor medicament, and provides a theoretical basis for subsequent research and development of drugs.

1 . A compound with anti-tumor activity, having the following structural formula: 
       
         
           
           
               
               
           
         
         wherein in the formula,
 R 1  is selected from hydroxyl, carboxyl, methyl, methoxy, and hydrogen; 
 R 2  is selected from vinyl, methyl, monochloromethyl, and phenyl; 
 R 3  is selected from carbomethoxy, ethoxycarbonyl, propoxycarbonyl, hydroxyl, methyl, and hydrogen; 
 R 4  is selected from hydrogen, hydroxyl, chloro, methyl, bromo, acetyl, carbomethoxy, and chloroacetamidomethyl; 
 R 5  is selected from hydroxyl, methyl, and hydrogen; 
 R 6  is selected from hydroxyl, acrylamidomethyl, acetamidomethyl, chloroacetamidomethyl, methyl, and hydrogen. 
 
       
     
     
         2 . The compound according to  claim 1 , wherein the compound is selected from the following compounds: 
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
     
     
         3 . A method for preparing the compound according to  claim 1 -er-2, comprising:
 allowing an aromatic compound and an amide compound in a molar ratio of 1:1.2˜2.4 to undergo a substitution reaction in an organic solvent at 25° C. to 55° C. for 48 hours to 96 hours in the presence of a catalyst, in which the molar ratio of the aromatic compound to the catalyst is 1:1.8˜1.9;   then carrying out filtration to obtain a solid product, and   thoroughly washing the solid product with deionized water and drying it to obtain the compound of chemical formula (I).   
     
     
         4 . The method according to  claim 3 , wherein the aromatic compound is gallic acid, methyl gallate, propyl gallate, 2,6-dihydroxytoluene, 3,5-dimethylanisole, 2,3,5-trimethylphenol, 4-chloro-3,5-dimethylphenol, 2,6-dihydroxyacetophenone, 2,4-dihydroxyacetophenone, 4-bromo-3,5-dihydroxybenzoic acid, or methyl 3,4-dihydroxybenzoate. 
     
     
         5 . The method according to  claim 3 , wherein the amide compound is N-hydroxymethyl acrylamide, N-hydroxymethyl acetamide, N-hydroxymethyl chloroacetamide, or N-hydroxymethyl benzamide. 
     
     
         6 . The method according to  claim 3 , wherein the catalyst is concentrated sulfuric acid or anhydrous aluminum trichloride. 
     
     
         7 . The method according to  claim 3 , wherein the solvent is dichloromethane, trichloromethane, acetone, or ethanol. 
     
     
         8 . The method according to  claim 3 , wherein the washed solid product is dried at a temperature of 50° C. to 60° C. for 360 minutes to 420 minutes, to obtain a dried solid product having a water content of 5% by weight or less. 
     
     
         9 . A method for treating cancer, comprising administering the compound of formula (I) according to  claim 1  to the subject. 
     
     
         10 . The method according to  claim 9 , wherein the cancer is lung cancer, liver cancer, colon cancer, leukemia, cervical cancer, or breast cancer.